CaltechAUTHORS
Published July 2, 2007 | Version Accepted Version + Supplemental Material
Journal Article Open

Completion of a Programmable DNA-Binding Small Molecule Library

Creators

  • 1. ROR icon California Institute of Technology

Abstract

Hairpin pyrrole-imidazole (Py-Im) polyamides are programmable oligomers that bind the DNA minor groove in a sequence-specific manner with affinities comparable to those of natural DNA-binding proteins. These cell-permeable small molecules have been shown to enter the nuclei of live cells and downregulate endogenous gene expression. We complete here a library of 27 hairpin Py-Im polyamides, which bind seven-base-pair sequences of the general form 5′-WWGNNNW-3′ (where W=A or T, N=W, G, or C). Their equilibrium association constants (K_a) range from K_a=1×10^8 to 4×10^(10) M^(−1) with good sequence specificity. A table of binding affinities and sequence contexts for this completed 27-member library has been assembled for the benefit of the chemical biology community interested in molecular control of transcription.

Additional Information

© 2007 Elsevier Ltd. Received 27 January 2007; revised 2 March 2007; accepted 6 March 2007; Available online 12 March 2007. We are grateful to the National Institutes of Health for research support.

Attached Files

Accepted Version - nihms25215.pdf

Supplemental Material - mmc1.pdf

Supplemental Material - mmc2.pdf

Supplemental Material - mmc3.pdf

Supplemental Material - mmc4.pdf

Supplemental Material - mmc5.pdf

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mmc1.pdf

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Additional details

Identifiers

PMCID
PMC2151752
Eprint ID
66750
DOI
10.1016/j.tet.2007.03.041
Resolver ID
CaltechAUTHORS:20160509-110446789

Related works

Describes
10.1016/j.tet.2007.03.041 (DOI)

Funding

NIH

Dates

Created
2016-05-17
Created from EPrint's datestamp field
Updated
2021-11-11
Created from EPrint's last_modified field